| Literature DB >> 30326403 |
Sushant K Shrivastava1, Saurabh K Sinha2, Pavan Srivastava3, Prabhash N Tripathi3, Piyoosh Sharma3, Manish K Tripathi3, Avanish Tripathi3, Priyanka K Choubey3, Digambar K Waiker3, Lalit M Aggarwal4, Manish Dixit5, Subhash C Kheruka5, Sanjay Gambhir5, Sharmila Shankar6, Rakesh K Srivastava7.
Abstract
Based on the quantitative structure-activity relationship (QSAR), some novel p-aminobenzoic acid derivatives as promising cholinesterase enzyme inhibitors were designed, synthesized, characterized and evaluated to enhance learning and memory. The in vitro enzyme kinetic study of the synthesized compounds revealed the type of inhibition on the respective acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vivo studies of the synthesized compounds exhibited significant reversal of cognitive deficits in the animal models of amnesia as compared to standard drug donepezil. Further, the ex vivo studies in the specific brain regions like the hippocampus, hypothalamus, and prefrontal cortex regions also exhibited AChE inhibition comparable to standard donepezil. The in silico molecular docking and dynamics simulations studies of the most potent compound 22 revealed the consensual interactions at the active site pocket of the AChE.Entities:
Keywords: Antiamnesic; Anticholinesterase; Molecular dynamics; Working and reference memory; p-Aminobenzoic acid
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Year: 2018 PMID： 30326403 DOI： 10.1016/j.bioorg.2018.10.009
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275